CA2831730A1 - A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation - Google Patents

A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation Download PDF

Info

Publication number
CA2831730A1
CA2831730A1 CA2831730A CA2831730A CA2831730A1 CA 2831730 A1 CA2831730 A1 CA 2831730A1 CA 2831730 A CA2831730 A CA 2831730A CA 2831730 A CA2831730 A CA 2831730A CA 2831730 A1 CA2831730 A1 CA 2831730A1
Authority
CA
Canada
Prior art keywords
compound
cancer
crystalline form
solvent
process according
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2831730A
Other languages
English (en)
French (fr)
Inventor
Suneel Manohar Babu Chennamsetty
Kishor JOSHI
Yogesh CHINCHWADE
Yogesh HULAWALE
Selvam PARAMASIVAN
Meenakshi Sivakumar
Sivaramakrishnan Hariharan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Piramal Enterprises Ltd
Original Assignee
Piramal Enterprises Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Piramal Enterprises Ltd filed Critical Piramal Enterprises Ltd
Publication of CA2831730A1 publication Critical patent/CA2831730A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2831730A 2011-04-21 2012-04-19 A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation Abandoned CA2831730A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161477937P 2011-04-21 2011-04-21
US61/477,937 2011-04-21
PCT/IB2012/051967 WO2012143879A1 (en) 2011-04-21 2012-04-19 A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation

Publications (1)

Publication Number Publication Date
CA2831730A1 true CA2831730A1 (en) 2012-10-26

Family

ID=46026953

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2831730A Abandoned CA2831730A1 (en) 2011-04-21 2012-04-19 A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
CA2833009A Abandoned CA2833009A1 (en) 2011-04-21 2012-04-19 Insulin-like growth factor-1 receptor inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2833009A Abandoned CA2833009A1 (en) 2011-04-21 2012-04-19 Insulin-like growth factor-1 receptor inhibitors

Country Status (9)

Country Link
US (3) US20140045832A1 (ja)
EP (2) EP2699568A1 (ja)
JP (1) JP2014514321A (ja)
CN (1) CN103732592A (ja)
AU (2) AU2012245455A1 (ja)
CA (2) CA2831730A1 (ja)
IL (1) IL228810A0 (ja)
IN (1) IN2013MN02170A (ja)
WO (3) WO2012143874A1 (ja)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103732592A (zh) * 2011-04-21 2014-04-16 默沙东公司 胰岛素样生长因子-1受体抑制剂
WO2014002007A1 (en) * 2012-06-26 2014-01-03 Piramal Enterprises Limited Method of predicting or monitoring response to igf-1r and ir inhibitors using biomarkers
JP6272897B2 (ja) 2012-11-29 2018-01-31 ケモセントリックス,インコーポレイティド Cxcr7アンタゴニスト
WO2014177915A1 (en) 2013-05-01 2014-11-06 Piramal Enterprises Limited Cancer combination therapy using imidazo[4,5-c]quinoline derivatives
CN104098498A (zh) * 2014-07-30 2014-10-15 天津市斯芬克司药物研发有限公司 一种吲唑类化合物及其制备方法
WO2016041953A1 (en) 2014-09-15 2016-03-24 Dmitry Gorilovsky A system comprising multiple digital cameras viewing a large scene
CN105218475A (zh) * 2015-10-15 2016-01-06 湖南华腾制药有限公司 1,2-吗啉盐酸盐的合成方法
CN111788191B (zh) * 2017-12-15 2024-06-04 英夕亚生物科技股份公司 用于治疗癌症的1-(哌啶基羰基甲基)-2-氧代哌嗪衍生物
BR112021011222A2 (pt) 2018-12-12 2021-08-24 Chemocentryx, Inc. Inibidores de cxcr7 para o tratamento de câncer
CN113149941A (zh) * 2020-01-22 2021-07-23 中国科学院上海药物研究所 醚类化合物及其在防治糖尿病及代谢综合征中的药学用途

Family Cites Families (309)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3126375A (en) 1964-03-24 Chioacyl
US2789118A (en) 1956-03-30 1957-04-16 American Cyanamid Co 16-alpha oxy-belta1, 4-pregnadienes
US2990401A (en) 1958-06-18 1961-06-27 American Cyanamid Co 11-substituted 16alpha, 17alpha-substituted methylenedioxy steroids
US3048581A (en) 1960-04-25 1962-08-07 Olin Mathieson Acetals and ketals of 16, 17-dihydroxy steroids
US3749712A (en) 1970-09-25 1973-07-31 Sigma Tau Ind Farmaceuti Triamcinolone acetonide esters and process for their preparation
US3996359A (en) 1972-05-19 1976-12-07 Ab Bofors Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith
SE378110B (ja) 1972-05-19 1975-08-18 Bofors Ab
SE378109B (ja) 1972-05-19 1975-08-18 Bofors Ab
US4294926A (en) 1979-06-15 1981-10-13 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4319039A (en) 1979-06-15 1982-03-09 Merck & Co., Inc. Preparation of ammonium salt of hypocholesteremic fermentation product
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
JPS5889191A (ja) 1981-11-20 1983-05-27 Sankyo Co Ltd 3−ヒドロキシ−ml−236b誘導体の製造法
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4911165A (en) 1983-01-12 1990-03-27 Ethicon, Inc. Pliabilized polypropylene surgical filaments
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4820850A (en) 1987-07-10 1989-04-11 Merck & Co., Inc. Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
US5180589A (en) 1988-03-31 1993-01-19 E. R. Squibb & Sons, Inc. Pravastatin pharmaceuatical compositions having good stability
US5030447A (en) 1988-03-31 1991-07-09 E. R. Squibb & Sons, Inc. Pharmaceutical compositions having good stability
US4916239A (en) 1988-07-19 1990-04-10 Merck & Co., Inc. Process for the lactonization of mevinic acids and analogs thereof
EP0360390A1 (en) 1988-07-25 1990-03-28 Glaxo Group Limited Spirolactam derivatives
US5290946A (en) 1988-10-13 1994-03-01 Sandoz Ltd. Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
US5118853A (en) 1988-10-13 1992-06-02 Sandoz Ltd. Processes for the synthesis of 3-disubstituted aminoacroleins
MX18467A (es) 1988-11-23 1993-07-01 Pfizer Agentes terapeuticos de quinuclidinas
US4929437A (en) 1989-02-02 1990-05-29 Merck & Co., Inc. Coenzyme Q10 with HMG-CoA reductase inhibitors
US5164372A (en) 1989-04-28 1992-11-17 Fujisawa Pharmaceutical Company, Ltd. Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same
US5189164A (en) 1989-05-22 1993-02-23 Sandoz Ltd. Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
IE903957A1 (en) 1989-11-06 1991-05-08 Sanofi Sa Aromatic amine compounds, their method of preparation and¹pharmaceutical compositions in which they are present
FR2654725B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2654726B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone et leur preparation.
GB8929070D0 (en) 1989-12-22 1990-02-28 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
UA41251C2 (uk) 1990-01-04 2001-09-17 Пфайзер, Інк. Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі
US5232929A (en) 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
WO1991012266A1 (en) 1990-02-15 1991-08-22 Fujisawa Pharmaceutical Co., Ltd. Peptide compound
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
EP0532527B1 (en) 1990-06-01 1994-11-09 Pfizer Inc. 3-amino-2-aryl quinuclidines, process for their preparation and pharmaceutical compositions containing them
PL167568B1 (pl) 1990-07-23 1995-09-30 Pfizer Sposób wytwarzania nowych pochodnych chinuklidyny PL PL
WO1994004494A1 (en) 1992-08-13 1994-03-03 Warner-Lambert Company Tachykinin antagonists
JPH0772175B2 (ja) 1990-09-28 1995-08-02 フアイザー・インコーポレイテツド 窒素含有非芳香族複素環の縮合環類似体
GB9023116D0 (en) 1990-10-24 1990-12-05 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
DK0498069T3 (da) 1990-12-21 1995-12-04 Fujisawa Pharmaceutical Co Ny anvendelse af peptidderivat
AU652407B2 (en) 1991-01-10 1994-08-25 Pfizer Inc. N-alkyl quinuclidinium salts as substance P antagonists
US5242930A (en) 1991-02-11 1993-09-07 Merck Sharp & Dohme Ltd. Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0573522B1 (en) 1991-03-01 1994-12-14 Pfizer Inc. 1-azabicyclo[3.2.2]nonan-3-amine derivatives
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
EP0581777A1 (en) 1991-03-26 1994-02-09 Pfizer Inc. Stereoselective preparation of substituted piperidines
FR2677361A1 (fr) 1991-06-04 1992-12-11 Adir Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
FR2676055B1 (fr) 1991-05-03 1993-09-03 Sanofi Elf Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676053B1 (fr) 1991-05-03 1993-08-27 Sanofi Elf Nouveaux composes dialkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676447B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole et leur preparation.
FR2676443B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole et leur preparation.
FR2676446B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2676442B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveau derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
DK0585328T3 (da) 1991-05-22 2002-02-11 Pfizer Substituerede 3-aminoquinuclidiner
WO1992020661A1 (en) 1991-05-22 1992-11-26 Merck & Co., Inc. N, n-diacylpiperazines
RU2103269C1 (ru) 1991-05-31 1998-01-27 Пфайзер Инк. Производные хинуклидина или их фармацевтически приемлемые соли и фармацевтическая композиция
GB9113219D0 (en) 1991-06-19 1991-08-07 Fujisawa Pharmaceutical Co Peptide compound,processes for preparation thereof and pharmaceutical composition comprising the same
UA39168C2 (uk) 1991-06-20 2001-06-15 Пфайзер, Інк. Фторалкоксифенільні похідні піперидину або хінуклідину, що є антагоністами речовини p і фармацевтична композиція на їх основі
TW202432B (ja) 1991-06-21 1993-03-21 Pfizer
US5288730A (en) 1991-06-24 1994-02-22 Merck Sharp & Dohme Limited Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0536817A1 (en) 1991-07-05 1993-04-14 MERCK SHARP & DOHME LTD. Azabicyclic compounds as tachykinin antagonists
US5472978A (en) 1991-07-05 1995-12-05 Merck Sharp & Dohme Ltd. Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
AU664188B2 (en) 1991-07-05 1995-11-09 Merck Sharp & Dohme Limited Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
CA2110725A1 (en) 1991-07-10 1993-01-21 Andrew P. Owens Aromatic compounds, compositions containing them and their use in therapy
WO1993001159A1 (en) 1991-07-10 1993-01-21 Merck Sharp & Dohme Limited Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy
MY110227A (en) 1991-08-12 1998-03-31 Ciba Geigy Ag 1-acylpiperindine compounds.
ATE136885T1 (de) 1991-08-20 1996-05-15 Merck Sharp & Dohme Azacyclische verbindungen, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen
ES2149767T5 (es) 1991-09-20 2005-06-16 Glaxo Group Limited Nuevo uso medico para antagonistas de taquiquininas.
DK0607164T3 (da) 1991-09-26 2002-06-17 Pfizer Kondenserede tricykliske nitrogenholdige heterocykliske forbindelser som substans P-receptorantagonister
WO1993009116A1 (en) 1991-11-07 1993-05-13 Yoshitomi Pharmaceutical Industries, Ltd. Quinuclidine compound and medicinal use thereof
ATE161821T1 (de) 1991-11-12 1998-01-15 Pfizer Azyklische ethylendiaminderivate als 'substance p rezeptor' antagonisten
EP0545478A1 (en) 1991-12-03 1993-06-09 MERCK SHARP & DOHME LTD. Heterocyclic compounds as tachykinin antagonists
HU9203780D0 (en) 1991-12-12 1993-03-29 Sandoz Ag Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them
GB9200535D0 (en) 1992-01-10 1992-02-26 Fujisawa Pharmaceutical Co New compound
GB9201179D0 (en) 1992-01-21 1992-03-11 Glaxo Group Ltd Chemical compounds
US5328927A (en) 1992-03-03 1994-07-12 Merck Sharpe & Dohme, Ltd. Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them
JP2656702B2 (ja) 1992-03-23 1997-09-24 ファイザー製薬株式会社 ペプチド性キヌクリジン
FR2689888B1 (fr) 1992-04-10 1994-06-10 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
EP0636130A1 (en) 1992-04-15 1995-02-01 Merck Sharp & Dohme Ltd. Azacyclic compounds
GB2266529A (en) 1992-05-01 1993-11-03 Merck Sharp & Dohme Tetrahydroisoquinoline derivatives
DE69331190T2 (de) 1992-05-18 2002-04-18 Pfizer Inc., New York Überbrückte azabicyclische derivate als substanz p antagonisten
GB9211193D0 (en) 1992-05-27 1992-07-08 Merck Sharp & Dohme Therapeutic agents
IL106142A (en) 1992-06-29 1997-03-18 Merck & Co Inc Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US5719147A (en) 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US5612336A (en) 1992-07-13 1997-03-18 Merck, Sharp & Dohme Ltd. Heterocyclic amide derivatives as tachykinin antagonists
EP1251170A3 (en) 1992-07-17 2002-10-30 Ribozyme Pharmaceuticals, Inc. Method and reagent for treatment of NF-kappaB dependent animal diseases
GB2268931A (en) 1992-07-22 1994-01-26 Merck Sharp & Dohme Azabicyclic tachykinin-receptor antagonists
WO1994002461A1 (en) 1992-07-28 1994-02-03 Merck Sharp & Dohme Limited Azacyclic compounds
GB2269170A (en) 1992-07-29 1994-02-02 Merck Sharp & Dohme Azatricyclic tachykinin antagonists
AU4718093A (en) 1992-07-31 1994-03-03 Merck Sharp & Dohme Limited Substituted amines as tachykinin receptor antagonists
CA2141051A1 (en) 1992-08-04 1994-02-17 Terry J. Rosen Substituted nitrogen-containing heterocycles
GB9216911D0 (en) 1992-08-10 1992-09-23 Merck Sharp & Dohme Therapeutic agents
AU4224993A (en) 1992-08-19 1994-03-15 Pfizer Inc. Substituted benzylamino nitrogen containing non-aromatic heterocycles
US5387595A (en) 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
DE69315920T2 (de) 1992-09-04 1998-06-10 Takeda Chemical Industries Ltd Kondensierte heterozyklische Verbindungen, deren Herstellung und Verwendung
AU4973693A (en) 1992-09-10 1994-03-29 Merck Sharp & Dohme Limited Alcohols and ethers with aromatic substituents as tachykinin-antagonists
GB9220286D0 (en) 1992-09-25 1992-11-11 Merck Sharp & Dohme Therapeutic agents
JP2656699B2 (ja) 1992-10-21 1997-09-24 ファイザー製薬株式会社 置換ベンジルアミノキヌクリジン
GB9222262D0 (en) 1992-10-23 1992-12-09 Merck Sharp & Dohme Therapeutic agents
GB9222486D0 (en) 1992-10-26 1992-12-09 Merck Sharp & Dohme Therapeutic agents
JP2656700B2 (ja) 1992-10-28 1997-09-24 ファイザー製薬株式会社 置換キヌクリジン誘導体
AU678409B2 (en) 1992-10-28 1997-05-29 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
AU5342894A (en) 1992-10-30 1994-05-24 Merck Sharp & Dohme Limited Tachykinin antagonists
KR950704311A (ko) 1992-11-12 1995-11-17 알렌 제이. 스피겔 물질 p 길항체로서의 퀴누클리딘 유도체(quinuclidine derivative as substance p antagonist)
US5261188A (en) 1992-11-23 1993-11-16 The Standard Products Company Belt weatherstrip with bulb
ATE194340T1 (de) 1992-12-10 2000-07-15 Pfizer Aminomethylen substituierte heterocyclische verbindungen und ihre verwendung alssubstanz p antagonisten
US5604260A (en) 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
EP0673367A1 (en) 1992-12-14 1995-09-27 MERCK SHARP & DOHME LTD. 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperidines as tachykinin receptor antagonists
GB9226581D0 (en) 1992-12-21 1993-02-17 Merck Sharp & Dohme Therapeutic agents
EP0604181A1 (en) 1992-12-21 1994-06-29 Eli Lilly And Company Antitumor compositions and method of treatment
GB9300051D0 (en) 1993-01-04 1993-03-03 Merck Sharp & Dohme Therapeutic agents
CA2297592A1 (en) 1993-01-15 1994-07-21 G.D. Searle & Co. Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
EP0610793A1 (en) 1993-02-08 1994-08-17 Takeda Chemical Industries, Ltd. Tetracyclic morpholine derivatives and their use or analgesics
WO1994019323A1 (en) 1993-02-18 1994-09-01 Merck Sharp & Dohme Limited Azacyclic compounds, compositions containing them and their use as tachykinin antagonists
AU6140694A (en) 1993-02-22 1994-09-14 Merck Sharp & Dohme Limited Aromatic compounds, compositions containing them and their use in therapy
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
US5298627A (en) 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
JP2832754B2 (ja) 1993-03-04 1998-12-09 ファイザー・インク. サブスタンスpアンタゴニストとしてのスピロアザ環式誘導体
US5409944A (en) 1993-03-12 1995-04-25 Merck Frosst Canada, Inc. Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
US5496833A (en) 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
NZ267209A (en) 1993-05-06 1997-09-22 Merrell Dow Pharma Substituted pyrrolidin-3-yl-alkyl-piperidine derivatives, preparation and pharmaceutical compositions thereof
EP0698015A1 (en) 1993-05-14 1996-02-28 Genentech, Inc. Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
IL109646A0 (en) 1993-05-19 1994-08-26 Pfizer Heteroatom substituted alkyl benzylamino-quinuclidines
US5380738A (en) 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
EP0702681A1 (en) 1993-06-07 1996-03-27 Merck & Co. Inc. Spiro-substituted azacycles as neurokinin antagonists
GB9602877D0 (en) 1996-02-13 1996-04-10 Merck Frosst Canada Inc 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5436265A (en) 1993-11-12 1995-07-25 Merck Frosst Canada, Inc. 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
ATE171945T1 (de) 1993-07-15 1998-10-15 Pfizer Benzyloxychinuclidine als substanz p antagonisten
GB9315808D0 (en) 1993-07-30 1993-09-15 Merck Sharp & Dohme Therapeutic agents
TW365603B (en) 1993-07-30 1999-08-01 Rhone Poulenc Rorer Sa Novel perhydroisoindole derivatives, their preparation and pharmaceutical compositions which contain them
GB9317987D0 (en) 1993-08-26 1993-10-13 Glaxo Group Ltd Chemical compounds
DK0719253T3 (da) 1993-09-17 2004-07-26 Pfizer 3-amino-5-carboxy-substituerede piperidiner og 3-amino-4-carboxy-substituerede pyrrolidiner som tachykininantagonister
EP1209157A1 (en) 1993-09-17 2002-05-29 Pfizer Inc. Heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethyl piperidines and related compounds
WO1995008542A1 (fr) 1993-09-22 1995-03-30 Kyowa Hakko Kogyo Co., Ltd. Inhibiteur de la farnesyl-transferase
IS4208A (is) 1993-09-22 1995-03-23 Glaxo Group Limited 3-(tetrazólýl-benzyl)amínó-piperadidín afleiður
ATE210652T1 (de) 1993-10-15 2001-12-15 Schering Corp Tricyclische carbamat-derivate zur inhibierung der g-protein funktion und für die behandlung von proliferativen erkrankungen
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
ZA947969B (en) 1993-10-15 1996-07-12 Schering Corp Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
WO1995011917A1 (en) 1993-10-25 1995-05-04 Parke, Davis & Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
AU7947594A (en) 1993-10-27 1995-05-22 Merck Sharp & Dohme Limited Substituted amides as tachykinin antagonists
US5344991A (en) 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
DE69417012T2 (de) 1993-11-04 1999-10-07 Abbott Laboratories, Abbott Park Cyclobutan-derivate als inhibitoren der squalen-synthetase und der protein-farnesyltransferase
JP3597863B2 (ja) 1993-11-05 2004-12-08 ワーナー−ランバート・コンパニー タンパク質:ファルネシルトランスフェラーゼの置換されたジ‐およびトリペプチド阻害剤
US6403577B1 (en) 1993-11-17 2002-06-11 Eli Lilly And Company Hexamethyleneiminyl tachykinin receptor antagonists
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
IT1271462B (it) 1993-12-03 1997-05-28 Menarini Farma Ind Antagonisti delle tachichinine,procedimento per la loro preparazione e loro impiego in formulazioni farmaceutiche.
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
JPH09506898A (ja) 1993-12-21 1997-07-08 イーライ・リリー・アンド・カンパニー 非ペプチドタキキニン受容体アンタゴニスト
CZ282567B6 (cs) 1993-12-29 1997-08-13 Pfizer Inc. Diazabicyklické sloučeniny a farmaceutické prostředky na jejich bázi
DE69434991T2 (de) 1993-12-29 2008-03-06 Merck Sharp & Dohme Ltd., Hoddesdon Substituierte Morpholinderivate und ihre Verwendung als Arzneimittel
ATE170174T1 (de) 1994-01-13 1998-09-15 Merck Sharp & Dohme Gem-bissubstituierte azazyclische tachykinin- antagonisten
JPH09508376A (ja) 1994-01-28 1997-08-26 メルク シヤープ エンド ドーム リミテツド アラルキル置換アザシクロ系の治療薬
US5393790A (en) 1994-02-10 1995-02-28 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
GB9402688D0 (en) 1994-02-11 1994-04-06 Merck Sharp & Dohme Therapeutic agents
US5610165A (en) 1994-02-17 1997-03-11 Merck & Co., Inc. N-acylpiperidine tachykinin antagonists
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
WO1995024612A1 (de) 1994-03-07 1995-09-14 International Business Machines Corporation Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper
HUT77406A (hu) 1994-03-15 1998-04-28 Eisai Co., Ltd., 1-(4-Amino-5-tio-pent-2-en)-il oldalláncot tartalmazó peptidomimetikumok és az ezeket tartalmazó gyógyszerkészítmények
FR2718136B1 (fr) 1994-03-29 1996-06-21 Sanofi Sa Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant.
IL113196A0 (en) 1994-03-31 1995-06-29 Bristol Myers Squibb Co Imidazole derivatives and pharmaceutical compositions containing the same
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5610145A (en) 1994-04-15 1997-03-11 Warner-Lambert Company Tachykinin antagonists
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
IL113472A0 (en) 1994-04-29 1995-07-31 Lilly Co Eli Non-peptidyl tachykinin receptor antogonists
US5747491A (en) 1994-05-05 1998-05-05 Merck Sharp & Dohme Ltd. Morpholine derivatives and their use as antagonists of tachikinins
CA2189764A1 (en) 1994-05-07 1995-11-16 Gerd Schnorrenberg Neurokinine (tachykinine) antagonists
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
CA2187531A1 (en) 1994-06-06 1995-12-14 David Christopher Horwell Tachykinin (nk1) receptor antagonists
CN1150419A (zh) 1994-06-10 1997-05-21 罗纳-布朗克罗莱尔股份有限公司 新的法呢基转移酶抑制剂、其制法及其药物组合物
EP0686629A3 (en) 1994-06-10 1999-02-10 Eli Lilly And Company Cyclohexyl tachykinine receptor antagonists
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
AU688072B2 (en) 1994-07-12 1998-03-05 Eli Lilly And Company Heterocyclic tachykinin receptor antagonists
CA2154116A1 (en) 1994-07-22 1996-01-23 Philip Arthur Hipskind 1-aryl-2-acetamidopentanone derivatives for use as tachykinin receptor antagonists
GB9415997D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9415996D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
TW432061B (en) 1994-08-09 2001-05-01 Pfizer Res & Dev Lactams
WO1996005529A1 (en) 1994-08-09 1996-02-22 Micron Optics, Inc. Temperature compensated fiber fabry-perot filters
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
DE69514367T2 (de) 1994-08-11 2000-07-27 Banyu Pharmaceutical Co., Ltd. Substituierte amidderivate
WO1996005169A1 (fr) 1994-08-12 1996-02-22 Banyu Pharmaceutical Co., Ltd. Derive d'acide amique n,n-bisubstitue
CA2195972A1 (en) 1994-08-15 1996-02-22 Merck Sharp & Dohme Limited Morpholine derivatives and their use as therapeutic agents
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
DE4429653C2 (de) 1994-08-20 1997-04-03 Anton Dr More Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl
EP0777666B1 (en) 1994-08-25 1999-03-03 Merrell Pharmaceuticals Inc. Substituted piperidines useful for the treatment of allergic diseases
DE69405864T2 (de) 1994-08-29 1998-03-26 Akzo Nobel Nv Verfahren zur Herstellung von quaternären Diestern
GB9417956D0 (en) 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9418545D0 (en) 1994-09-15 1994-11-02 Merck Sharp & Dohme Therapeutic agents
US5457107A (en) 1994-09-16 1995-10-10 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
CA2198382A1 (en) 1994-09-30 1996-04-11 Novartis Ag 1-acyl-4-aliphatylaminopiperidine compounds
TW397825B (en) 1994-10-14 2000-07-11 Novartis Ag Aroyl-piperidine derivatives
FR2725986B1 (fr) 1994-10-21 1996-11-29 Adir Nouveaux derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE69534213T2 (de) 1994-10-25 2006-01-12 Astrazeneca Ab Therapeutisch wirksame Heterocyclen
GB9421709D0 (en) 1994-10-27 1994-12-14 Zeneca Ltd Therapeutic compounds
EP0740853B1 (en) 1994-11-22 1999-01-13 Koninklijke Philips Electronics N.V. Semiconductor device with a carrier body on which a substrate with a semiconductor element is fastened by means of a glue layer and on which a pattern of conductor tracks is fastened
CA2162786A1 (en) 1994-11-22 1996-05-23 Philip Arthur Hipskind Heterocyclic tachykinin receptor antagonists
FR2727411B1 (fr) 1994-11-30 1997-01-03 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent
AU3971295A (en) 1994-12-09 1996-06-26 Warner-Lambert Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
PE38997A1 (es) 1994-12-13 1997-10-02 Novartis Ag Antagonista de taquicinina
GB9426103D0 (en) 1994-12-23 1995-02-22 Merck Sharp & Dohme Therapeutic agents
WO1996021701A2 (en) 1995-01-09 1996-07-18 Magla International Ltd. Wear resistant image printing on latex surfaces
JP3925662B2 (ja) 1995-01-12 2007-06-06 グラクソ,グループ,リミテッド タキキニンアンタゴニスト活性を有するピペリジン誘導体
EP0794789A4 (en) 1995-01-12 1999-05-26 Univ Pittsburgh PRENYL TRANSFERASE INHIBITORS
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2729951B1 (fr) 1995-01-30 1997-04-18 Sanofi Sa Nouveaux composes heterocycliques, procede pour leur preparation et compositions pharmaceutiques en contenant
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5633272A (en) 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
GB9505491D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9505492D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
US5554641A (en) 1995-03-20 1996-09-10 Horwell; David C. Nonpeptides as tachykinin antagonists
GB9505692D0 (en) 1995-03-21 1995-05-10 Glaxo Group Ltd Chemical compounds
EP0733632B1 (en) 1995-03-24 2003-06-04 Takeda Chemical Industries, Ltd. Cyclic compounds, their production and use as tachykinin receptor antagonists
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5565568A (en) 1995-04-06 1996-10-15 Eli Lilly And Company 2-acylaminopropanamides as tachykinin receptor antagonists
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
EP0820452B1 (en) 1995-04-07 2003-06-04 Schering Corporation Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase
EP0830347B1 (en) 1995-04-13 2004-09-22 Aventis Pharmaceuticals, Inc. Novel substituted piperazine derivatives having tachykinin receptor antagonists activity
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
CN1072220C (zh) 1995-05-25 2001-10-03 藤泽药品工业株式会社 作为神经激肽受体拮抗剂的1-苯甲酰基-2-(吲哚基-3-烷基)-哌嗪衍生物
WO1997000252A1 (en) 1995-06-16 1997-01-03 Warner-Lambert Company Tricyclic inhibitors of protein farnesyltransferase
GB9513121D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513117D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513118D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
ES2155601T3 (es) 1995-07-07 2001-05-16 Pfizer Compuestos de benzolactama sustituidos como antagonistas de la sustancia p.
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
AT402617B (de) 1995-07-11 1997-07-25 Datacon Schweitzer & Zeindl Gm Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
TW340842B (en) 1995-08-24 1998-09-21 Pfizer Substituted benzylaminopiperidine compounds
US6020343A (en) 1995-10-13 2000-02-01 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
JP2002534955A (ja) 1995-10-18 2002-10-15 メルク エンド カンパニー インコーポレーテッド シクロペンチルタキキニン受容体アンタゴニスト
ES2196186T3 (es) 1995-11-06 2003-12-16 Univ Pittsburgh Inhibidores de protein-isoprenil-transferasas.
DE19541283A1 (de) 1995-11-06 1997-05-07 Boehringer Ingelheim Kg Neue Aminosäurederivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
GB9523244D0 (en) 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
EP1440973A3 (de) 1995-11-17 2004-10-20 Gesellschaft für biotechnologische Forschung mbH (GBF) Epothilonderivate, Herstellung und Mittel
WO1997018813A1 (en) 1995-11-22 1997-05-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6060469A (en) 1995-11-23 2000-05-09 Merck Sharp & Dohme Ltd. Spiro-piperidine derivatives and their use as tachykinin antagonists
GB9524157D0 (en) 1995-11-25 1996-01-24 Pfizer Ltd Therapeutic agents
HU224225B1 (hu) 1995-12-01 2005-06-28 Sankyo Co. Ltd. Tachikinin receptor antagonista hatású heterociklusos vegyületek, ezek előállítási eljárása és alkalmazásuk gyógyszerkészítmények előállítására
DE69620445T2 (de) 1995-12-08 2002-12-12 Janssen Pharmaceutica N.V., Beerse (imidazol-5-yl)methyl-2-chinolinoderivate als farnesyl protein transferase inhibitoren
GB9525296D0 (en) 1995-12-11 1996-02-07 Merck Sharp & Dohme Therapeutic agents
JP3193725B2 (ja) 1995-12-22 2001-07-30 シェーリング コーポレイション G―タンパク質機能の阻害および増殖性疾患の処置に有用な三環式アミド
WO1997026246A1 (en) 1996-01-16 1997-07-24 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
WO1997038665A2 (en) 1996-04-03 1997-10-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP1288206B1 (en) 1996-04-12 2008-09-17 G.D. Searle LLC Substituted benzenesulfonamide derivatives as prodrugs of COX-2 inhibitors
NZ332712A (en) 1996-05-22 2000-07-28 Warner Lambert Co Polypeptide inhibitors of protein farnesyl transferase
EP0918771A4 (en) 1996-07-15 2001-02-07 Bristol Myers Squibb Co THIADIOXOBENZODIAZEPINES FOR USE AS FARNESYL PROTEIN TRANSFERASE INHIBITORS
US5861419A (en) 1996-07-18 1999-01-19 Merck Frosst Canad, Inc. Substituted pyridines as selective cyclooxygenase-2 inhibitors
DE69734362T2 (de) 1996-12-03 2006-07-20 Sloan-Kettering Institute For Cancer Research Synthese von epothilonen, zwischenprodukte dazu, analoga und verwendungen davon
JP2001507699A (ja) 1996-12-30 2001-06-12 メルク エンド カンパニー インコーポレーテッド ファルネシル蛋白トランスフェラーゼ阻害薬
AU6013998A (en) 1996-12-30 1998-07-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO2000044777A1 (en) 1999-01-29 2000-08-03 Imclone Systems Incorporated Antibodies specific to kdr and uses thereof
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
EP1187633A4 (en) 1999-04-08 2005-05-11 Arch Dev Corp USE OF ANTI-VEGF ANTIBODY FOR INCREASING IRRADIATION IN CANCER THERAPY
KR20020062930A (ko) 1999-10-27 2002-07-31 싸이토키네틱스, 인코포레이티드 퀴나졸리논을 사용하는 방법 및 조성물
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
WO2002083140A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
ATE400274T1 (de) 2001-04-10 2008-07-15 Merck & Co Inc Hemmstoffe der akt aktivität
WO2002083675A2 (en) 2001-04-10 2002-10-24 Merck Sharp & Dohme Limited Inhibitors of akt activity
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2003013526A1 (en) 2001-08-08 2003-02-20 Merck & Co. Inc. Anticoagulant compounds
CA2465491A1 (en) 2001-11-07 2003-05-15 Merck & Co., Inc. Mitotic kinesin inhibitors
US7262186B2 (en) 2001-12-06 2007-08-28 Merck & Co., Inc. Substituted pyrazolo[3,4-d] pyrimidinones as a mitotic kinesin inhibitor
ATE424388T1 (de) 2001-12-06 2009-03-15 Merck & Co Inc Mitotische kinesinhemmer
DE60222302T2 (de) 2001-12-06 2008-05-29 Merck & Co., Inc. Inhibitoren von mitotischem kinesin
AU2002364128B2 (en) 2001-12-06 2008-03-06 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
ATE447577T1 (de) 2001-12-06 2009-11-15 Merck & Co Inc Mitotische kinesin-hemmer
KR100956195B1 (ko) 2002-02-01 2010-05-06 어리어드 파마슈티칼스, 인코포레이티드 인 함유 화합물 및 이의 용도
JP4399269B2 (ja) 2002-03-08 2010-01-13 メルク エンド カムパニー インコーポレーテッド 有糸分裂性キネシン阻害薬
CA2480880C (en) 2002-04-08 2011-03-22 Merck & Co., Inc. Inhibitors of akt activity
WO2003086394A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
JP4394959B2 (ja) 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害剤
US7273869B2 (en) 2002-04-08 2007-09-25 Merck & Co., Inc. Inhibitors of Akt activity
CA2483627A1 (en) 2002-05-23 2003-12-04 Merck & Co., Inc. Mitotic kinesin inhibitors
CA2485343A1 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
US7301028B2 (en) 2002-06-14 2007-11-27 Merck & Co., Inc. Mitotic kinesin inhibitors
MXPA04012642A (es) 2002-06-14 2005-03-23 Merck & Co Inc Inhibidores de la cinesina mitotica.
CA2494962C (en) * 2002-08-09 2011-06-14 Merck & Co., Inc. Tyrosine kinase inhibitors
AR046639A1 (es) 2003-11-21 2005-12-14 Schering Corp Combinaciones terapeuticas de anticuerpo anti- igfr1
EP1863571A1 (en) 2005-03-09 2007-12-12 Shering Corporation Compounds for inhibiting ksp kinesin activity
WO2006098961A2 (en) 2005-03-09 2006-09-21 Schering Corporation Fused thieno [2, 3-b] pyridine and thiazolo [5, 4-b] pyridine compounds for inhibiting ksp kinesin activity
CA2621820A1 (en) * 2005-09-09 2007-03-15 Jan Gunzinger Isoquinolines derivatives as igf-1r inhibitors
DE602006021327D1 (de) * 2005-09-09 2011-05-26 Analytecon Sa Isochinoline als igf-1r-inhibitoren
DK1966151T3 (da) 2005-12-13 2012-01-30 Schering Corp Polycykliske indazolderivater, der er ERK-hæmmere
CN101415674A (zh) 2006-02-16 2009-04-22 先灵公司 作为erk抑制剂的吡咯烷衍生物
CN101772501A (zh) 2007-06-18 2010-07-07 先灵公司 杂环化合物及其作为erk抑制剂的用途
CN103732592A (zh) * 2011-04-21 2014-04-16 默沙东公司 胰岛素样生长因子-1受体抑制剂

Also Published As

Publication number Publication date
EP2699567A1 (en) 2014-02-26
WO2012143874A1 (en) 2012-10-26
IL228810A0 (en) 2013-12-31
WO2012145471A1 (en) 2012-10-26
AU2012245971A1 (en) 2013-10-17
AU2012245971A8 (en) 2013-11-07
CA2833009A1 (en) 2012-10-26
JP2014514321A (ja) 2014-06-19
WO2012143879A1 (en) 2012-10-26
IN2013MN02170A (ja) 2015-06-12
AU2012245455A1 (en) 2013-10-31
AU2012245455A8 (en) 2013-11-07
CN103732592A (zh) 2014-04-16
US20140045832A1 (en) 2014-02-13
US20140046059A1 (en) 2014-02-13
EP2699568A1 (en) 2014-02-26
US20140045847A1 (en) 2014-02-13

Similar Documents

Publication Publication Date Title
CA2831730A1 (en) A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
JP7383652B2 (ja) B-rafキナーゼのマレイン酸塩、結晶形、調整方法、及びその使用
AU2017311645B2 (en) Pyridopyrimdinone CDK2/4/6 inhibitors
JP2022058514A (ja) メニン-mll相互作用の阻害剤
DK2763992T3 (en) NOVEL CHIRAL N-acyl-5,6,7, (8-substituted) -tetrahydro [1,2,4] triazolo [4,3-a] pyrazines as selective NK-3 receptor antagonists, PHARMACEUTICAL COMPOSITION AND METHODS FOR THE use in the NK-3 receptor mediated diseases
WO2022206723A1 (zh) 杂环类衍生物、其制备方法及其医药上的用途
WO2018045956A1 (zh) 苯并咪唑类化合物激酶抑制剂及其制备方法和应用
EA027563B1 (ru) Пиридопиразины, обладающие противораковой активностью через ингибирование fgfr киназ
CN112638917A (zh) 作为激酶抑制剂的杂环化合物、包括该杂环化合物的组合物、及其使用方法
JP2008514628A (ja) 蛋白質キナーゼ類のイミダゾ{4,5−b}ピラジノン阻害剤
KR20110075010A (ko) 키나제 억제제로서 유용한 이미다조피리다진카르보니트릴
AU2013354552B2 (en) Substituted pyridopyrazines as Syk inhibitors
GB2563642A (en) Small molecule modulators of human STING
JP2019534857A (ja) 神経保護作用、自己免疫性ならびに癌の疾患および病状において有用な1,2−ジチオラン化合物
TWI555745B (zh) 喹唑啉-7-醚化合物及其使用方法
WO2011071716A1 (en) Heterocyclic compounds containing an indole core
CA3136224A1 (en) Condensed azines for ep300 or cbp modulation and indications therefor
WO2018214866A1 (zh) 一种氮杂芳基衍生物、其制备方法和在药学上的应用
JP5978302B2 (ja) リゾホスファチジン酸アンタゴニストとしての(n−ベンズイミダゾール−2−イル)−シクロプロパンカルボキサミド
JP5583845B2 (ja) イミダゾピリダジニル化合物および癌に対するそれらの使用
CN114746419B (zh) N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途
KR20170030550A (ko) 퀴녹살린 화합물, 그것의 제조 방법 및 용도
RU2807277C2 (ru) Соединения пиримидина и содержащие их фармацевтические композиции для предупреждения или лечения рака
TWI707853B (zh) 1,2-二氫-1,6-萘啶類衍生物、其製備方法、其藥物組合物及其在醫藥上的用途
JP6715921B2 (ja) キナーゼ阻害剤および癌治療におけるそれらの使用

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20160420